Aims The present pharmacokinetic study was undertaken to determine the dose proportionality of three different doses of budesonide-400 mg, 800 mg or 1600 mg administered twice daily by a dry-powder inhaler (TurbuhalerA) in adult patients with mild asthma. Methods A total of 38 patients received budesonide by inhalation, 13 received 400 mg twice daily, 12 received 800 mg twice daily and 13 received 1600 mg twice daily. Mean FEV 1 at inclusion was 3.4, 4.0 and 3.9 l min −1 in the three groups,respectively. Blood samples were taken after a single dose, and after 3 weeks of daily treatment, for pharmacokinetic evaluation. Plasma concentrations of budesonide were determined by liquid chromatography plus mass spectrometry.Results Eleven evaluable patients remained in each dose group. Mean time to peak budesonide plasma concentration (t max ) was short (0.28-0.40 h) and did not differ between treatment groups. Budesonide concentrations declined rapidly thereafter, indicating efficient pulmonary absorption and rapid elimination with a half-life of approximately 3 h. C max was 1.4(2.0) nmol l −1 (single (repeated) doses), 2.6(3.6) nmol l −1 and 5.4(6.4) nmol l −1 after 400, 800 and 1600 mg twice daily, respectively. The corresponding results for the area under the plasma concentration vs time curve (AUC) were 271(325), 490(628) and 915(1096) nmol l −1 min. Ninety percent confidence intervals for pairwise dose-normalized C max and AUC comparisons between groups were large but contained unity in all cases, thus indicating dose-proportional pharmacokinetics. Regression on analysis supported these findings. Mean AUC after repeated doses (AUC(0,12 h,RD)) was on average 23% higher than the mean AUC after single doses (AUC(0,2,SD)( P=0.04) with no significant differences between doses, indicating slight accumulation following bid dosing. Conclusions In this relatively small study, budesonide inhaled via TurbuhalerA appeared to have dose-proportional pharmacokinetics, both within and above the clinically recommended dose range for asthmatic patients.Keywords: budesonide, pharmacokinetics, TurbuhalerA orally. This is because the inhaled drug acts locally, so a Introduction lower dose can be employed, which reduces systemic exposure and results in fewer side effects [1]. As a Over the last four decades, glucocorticosteroids (GCS) have been the most effective therapy available for the consequence of the improved safety profile, inhaled steroids are now commonly used across a wide spectrum maintenance treatment of asthma. Unfortunately, oral administration of GCS is often associated with a high of asthma severity. Budesonide was developed to further enhance topical incidence of systemic side effects. Inhaled GCS have a better ratio of local to systemic effects than those given anti-inflammatory effects while minimizing the systemic effects observed with other GCS. Both preclinical and clinical studies with inhaled budesonide have demon- activity and systemic GCS effect over a wide range of